Results for Antibiotics & Metabolites ( 217 )
Activity: Antibiotic . Function/Pharmacology: Mupirocin is a topical antibiotic/antibacterial.1 It inhibits isoleucyl-tRNA synthase. High level mupirocin resistance was found in 8.2% of Staphylococcus aureus and 15.6% of coagulase-negative staphylococci with high level resistance being more common in methicillin-sensitive S. aureus in comparison with methicillin-resistant S. aureus.2
Activity: Endogenous cholesterol metabolite . Function/Pharmacology: 24(S)-Hydroxycholesterol is an important cholesterol metabolite (cholesterol 24-hydroxylase) found in the brain.1 It is an endogenous agonist of the nuclear receptor LXR.2 It has been shown to induce cell death in neuroblastoma cells3, possibly via a necroptosis pathway4. 24(S)-Hydroxycholesterol has also been found to be a high affinity ligand for RORα and RORγ (Ki = 25 nM).5 24(S)-Hydroxycholesterol levels are elevated in the cerebral spinal fluids of patients with neurogenerative diseases suggesting possible clinical applications.6,7 It was also able to reduce Aβ production and increase ER-resident immature amyloid precursor protein (APP) levels in human neuroblastoma SH-Sy5Y cells and CHO cells via inhibition of intracellular amyloid precursor protein trafficking.7
Activity: Antibiotic and FOXM1 inhibitor . Function/Pharmacology: Novel cyclopeptide antibiotic. Blocks bacterial protein synthesis by inhibition of mRNA-tRNA translocation by GTPase elongation factor G (EF-G), EF-TU(GTP)-catalyzed aa-tRNA delivery as well as the activity of initiation factor-1 (IF-2)1-2. Displays antitumor activity. Induces apoptosis and cell cycle arrest in various tumor cells via downregulation of FOXM1 expression3. Chemical Name: Fermentation product from Streptomyces azureus
Activity: Risperidone metabolite . Function/Pharmacology: Pharmacologically active metabolite of risperidone, an atypical antipsychotic agent.1 Displays high affinity for serotonin 5-HT2A receptors as well as dopamine D2 receptors.2,3 Chemical Name: 3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
Activity: Quetiapine metabolite . Function/Pharmacology: Pharmacologically active metabolite of quetiapine.1 Exhibits distinct pharmacological activity from quetiapine and plays an important role in its antidepressant activity.2 Activates ERK1/2 and induces release of BDNF in C6 glioma cells which may contribute to the antidepressant properties of quetiapine.3 Inhibits the norepinephrine transporter which may contribute to the antipsychotic activity of quetiapine.4 Chemical Name: 11-(1-Piperazinyl)-dibenzo[b,f][1,4]thiazepine dihydrochloride
Activity: Fluoxetine metabolite . Function/Pharmacology: Metabolite of fluoxetine.3 Induces long QT syndrome via slow delayed rectifier potassium current block.1 Time dependent inhibitor of CYP2C19 and CYP3A4.2 The S-isomer of desmethylfluoxetine is the active N-demethylated metabolite responsible for the persistently potent and selective inhibition of serotonin uptake in vivo.3 Potent inhibitor of coxsackievirus replication acting via inhibition of viral RNA synthesis.4 State-dependent TREK-2 blocker.5 Chemical Name: 3-Phenyl-3-(4-trifluoromethyl-phenoxy)-propylamine hydrochloride (racemic)